AR033382A1 - OPHTHALM FORMULATION OF A SELECTIVE DRUG FOR THE INHIBITION OF CYCLOOXYGENASA-2 - Google Patents

OPHTHALM FORMULATION OF A SELECTIVE DRUG FOR THE INHIBITION OF CYCLOOXYGENASA-2

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Publication number
AR033382A1
AR033382A1 ARP010103304A ARP010103304A AR033382A1 AR 033382 A1 AR033382 A1 AR 033382A1 AR P010103304 A ARP010103304 A AR P010103304A AR P010103304 A ARP010103304 A AR P010103304A AR 033382 A1 AR033382 A1 AR 033382A1
Authority
AR
Argentina
Prior art keywords
eye
composition
inhibition
cox
disorder
Prior art date
Application number
ARP010103304A
Other languages
Spanish (es)
Inventor
Leslie C Hawley
Paramita Bandyopadhyay
Tugrul T Kararli
Satish Singh
Original Assignee
Upjohn Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Upjohn Co filed Critical Upjohn Co
Publication of AR033382A1 publication Critical patent/AR033382A1/en

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    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51—Nanocapsules; Nanoparticles
    • A61K9/5107—Excipients; Inactive ingredients
    • A61K9/513—Organic macromolecular compounds; Dendrimers
    • A61K9/5138—Organic macromolecular compounds; Dendrimers obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/12—Ketones
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    • A61K31/12—Ketones
    • A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
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    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
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Abstract

Una composicion farmacéutica que contiene una droga de baja solubilidad en agua y que se utiliza a través de la aplicacion topica en el ojo para el tratamiento o la prevencion de un desorden o una enfermedad oftálmica y en particular con una formulacion oftálmica de una droga selectiva para la inhibicion de ciclooxigenasa-2, que puede ser aplicada en el ojo para el tratamiento o la prevencion de un desorden o una enfermedad oftálmica vinculada con la ciclooxigenasa-2. El campo de la presente incluye, además del uso terapéutico o profiláctico de dicha composicion, el uso de dicha composicion en la preparacion de un medicamento. Una composicion farmacéutica adecuada para la administracion topica en el ojo, que comprende una droga selectiva para la inhibicion de COX-2 o una sal o prodroga de la misma en una concentracion efectiva para el tratamiento y/o profilaxis de un desorden en el ojo, y uno o más ingredientes excipientes oftálmicamente aceptables que reducen la cantidad de composicion que sale del ojo a través de la accion de lagrimar de manera tal que la composicion tiene un tiempo efectivo de permanencia en el ojo de 2 a 24 horas. Dicha composicion donde la droga selectiva para la inhibicion de COX-2 es de baja solubilidad en agua y es un compuesto de la formula (1) donde R3 es un grupo imida, amino o metilo, R4 es un hidrogeno o un grupo alcoxi o alquilo de C1-4, X es N o CR5 donde R5 es hidrogeno o halogeno, y Y y Z son independientemente átomos de carbono o nitrogeno que definen átomos adyacentes de un anillo de cinco a seis miembros, sustituido o no sustituido a una o más posiciones con grupos oxo, halo, metilo o halometilo; o una prodroga de dicho compuesto. Dicha composicion presenta la forma seleccionada de soluciones, suspensiones o solucion/suspenciones que son gelificables in situ al momento de aplicacion en el ojo; unguentos; y artículos solidos adecuados para el implante ocular. Dicha composicion comprende de 0,01% a 50% en peso/volumen de la droga selectiva para la inhibicion de COX- 2. Dicha composicion donde el tamano medio de la partícula de la droga es de 500 a 900 nm. Dicha composicion donde (a) comprende de 0,1% a 6,5% en peso de uno o más polímeros que contienen carboxilo ligeramente cruzados, (b) tiene un pH de 3 a 6.5 y una viscosidad inicial, cuando se la administra en el ojo, de 1000 a 30.000 cPs, y (c) se gelifica cuando entra en contacto con la secrecion lagrimal que tiene un pH de 7,2 a 7,4. Un método de tratamiento y o prevencion de un desorden vinculado con la COX-2 en el ojo de un mamífero, que comprende la administracion de una o más de las aplicaciones topicas de una cantidad terapéutica o profilácticamente efectiva de dicha droga selectiva para la inhibicion de COX-2 o luna sal o prodroga de la misma. Dicho método donde el mamífero es un ser humano. Un método para la elaboracion de un medicamento para el tratamiento o prevencion topica de un desorden en el ojo, que comprende la utilizacion de una composicion que comprende dicha droga selectiva para la inhibicion de COX-2 o una sal o prodroga de la misma. Una composicion farmacéutica adecuada para la administracion topica en el ojo, que comprende nanopartículas de una droga de baja solubilidad en agua en una concentracion efectiva para el tratamiento y/o la profilaxis de un desorden en el ojo.A pharmaceutical composition containing a drug of low water solubility and that is used through topical application in the eye for the treatment or prevention of a disorder or an ophthalmic disease and in particular with an ophthalmic formulation of a selective drug for the inhibition of cyclooxygenase-2, which can be applied in the eye for the treatment or prevention of an ophthalmic disorder or disease linked to cyclooxygenase-2. The field herein includes, in addition to the therapeutic or prophylactic use of said composition, the use of said composition in the preparation of a medicament. A pharmaceutical composition suitable for topical administration in the eye, comprising a selective drug for the inhibition of COX-2 or a salt or prodrug thereof in an effective concentration for the treatment and / or prophylaxis of a disorder in the eye, and one or more ophthalmically acceptable excipient ingredients that reduce the amount of composition that leaves the eye through the tearing action such that the composition has an effective time in the eye of 2 to 24 hours. Said composition where the selective drug for COX-2 inhibition is of low water solubility and is a compound of the formula (1) where R3 is an imide, amino or methyl group, R4 is a hydrogen or an alkoxy or alkyl group C1-4, X is N or CR5 where R5 is hydrogen or halogen, and Y and Z are independently carbon or nitrogen atoms that define adjacent atoms of a five to six membered ring, substituted or unsubstituted to one or more positions with oxo, halo, methyl or halomethyl groups; or a prodrug of said compound. Said composition presents the selected form of solutions, suspensions or solution / suspensions that are gellable in situ at the time of application in the eye; ointments; and solid articles suitable for the eye implant. Said composition comprises from 0.01% to 50% by weight / volume of the selective drug for COX-2 inhibition. Said composition where the average size of the drug particle is 500 to 900 nm. Said composition where (a) comprises from 0.1% to 6.5% by weight of one or more polymers containing slightly crossed carboxyl, (b) has a pH of 3 to 6.5 and an initial viscosity, when administered in the eye, from 1000 to 30,000 cPs, and (c) gels when it comes in contact with the tear secretion that has a pH of 7.2 to 7.4. A method of treatment and prevention of a disorder linked to COX-2 in the eye of a mammal, comprising the administration of one or more of the topical applications of a therapeutic or prophylactically effective amount of said selective drug for COX inhibition. -2 or moon salt or prodrug thereof. Said method where the mammal is a human being. A method for the preparation of a medicament for the treatment or topical prevention of a disorder in the eye, comprising the use of a composition comprising said selective drug for the inhibition of COX-2 or a salt or prodrug thereof. A pharmaceutical composition suitable for topical administration in the eye, comprising nanoparticles of a drug of low water solubility in an effective concentration for the treatment and / or prophylaxis of a disorder in the eye.

ARP010103304A 2000-07-13 2001-07-12 OPHTHALM FORMULATION OF A SELECTIVE DRUG FOR THE INHIBITION OF CYCLOOXYGENASA-2 AR033382A1 (en)

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